BR9506559C8 - compounds of tetracyclic derivatives, cis isomer of tetracyclic derivatives, and pharmaceutical composition - Google Patents

compounds of tetracyclic derivatives, cis isomer of tetracyclic derivatives, and pharmaceutical composition

Info

Publication number
BR9506559C8
BR9506559C8 BRPI9506559A BR9506559A BR9506559C8 BR 9506559 C8 BR9506559 C8 BR 9506559C8 BR PI9506559 A BRPI9506559 A BR PI9506559A BR 9506559 A BR9506559 A BR 9506559A BR 9506559 C8 BR9506559 C8 BR 9506559C8
Authority
BR
Brazil
Prior art keywords
alkyl
compound
pharmaceutical composition
ring
represents hydrogen
Prior art date
Application number
BRPI9506559A
Other languages
Portuguese (pt)
Other versions
BR9506559A (en
Inventor
Claude-Marie Daugan Alain
Original Assignee
Icos Corp
Laboratoire Glaxo Wellcome S A
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10749089&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR9506559(C8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Icos Corp, Laboratoire Glaxo Wellcome S A filed Critical Icos Corp
Publication of BR9506559A publication Critical patent/BR9506559A/en
Publication of BR9506559C8 publication Critical patent/BR9506559C8/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Abstract

patente de invenção "composto, isômero cis, uso de um composto, processo para o tratamento de angina estável, instável e variável, hipertensão, hipertensão pulmonar, doença pulmonar obstrutiva crônica, falha cardíaca congestiva, falha renal, aterosclerose, estados doentios de desobstrução reduzida de vasos sanguíneos, doenças vascular periférica, distúrbios vasculares, doenças inflamatórias, ataque cardíaco, bronquite, asma crônica, asma alérgica, rinite alérgica, glaucoma ou doenças de distúrbios na mobilidade intestinal, em um corpo animal humano ou não-humano, composição farmacêutica, processo para a preparação de uma composição farmacêutica, e, processo para preparar um composto". composto da f#romula (i) e seus sais e solvatos, em que: r^ 0^ representa hidrogênio ou alquila c~ 1-6~; r^ 1^ representa hidrogênio, alquila c~ 1-6~, alquenila c~ 2-6~, alquinila c~ 2-6~ halo alquila c~ 1-6~, cicloalquila c~ 3-8~, cicloalqula c~ 3-8~ alquila c~ 1-3~, aril alquila c~ 1-3~ ou heteroaril alquila c~ 1-3~; r^ 2^ representa um anel aromático monocíclico opcionalmente substituído selecionado dentre benzeno, tiofeno, furano e piridina ou um anel bicíclico opcionalmente substitído (a) fixado ao resto da molécula via um dos átomos de carbono do anel benzeno e em que o anel fundido (a) é um anel de 5 ou 6 membros que pode ser saturado ou parcialmente ou completamente insaturado e compreende átomos de carbono e opcionalmente um ou dois heteroátomos selecionados dente oxigênio, enxofre e nitrogênio; r^ 3^ representa hidrogênio ou alquila c~ 1~- c~ 3~, ou r^ 1^ e r^ 3^ juntos, representam uma cadeia alquenila ou alquila de 3 ou 4 membros. um composto da fórmula (i) é um inibidor potente e seletivo de fosfodiesterase específico de 3', 5' monofostato de guanosina cíclica (pde específico de cgmp) tendo uma utilidade em uma variedade de área terapêuticas onde tal inibição é benéfica, incluindo o tratamento de distúrbios cardiovasculares.invention patent "compound, cis isomer, use of a compound, process for the treatment of stable, unstable and variable angina, hypertension, pulmonary hypertension, chronic obstructive pulmonary disease, congestive heart failure, renal failure, atherosclerosis, sick states of reduced clearance blood vessels, peripheral vascular diseases, vascular disorders, inflammatory diseases, heart attack, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma or diseases of intestinal mobility disorders, in a human or non-human animal body, pharmaceutical composition, process for preparing a pharmaceutical composition, and process for preparing a compound ". compound of formula # (i) and its salts and solvates, wherein: r ^ 0 ^ represents hydrogen or c ~ 1-6 ~ alkyl; r ^ 1 ^ represents hydrogen, c ~ 1-6 ~ alkyl, c ~ 2-6 ~ alkenyl, c ~ 2-6 ~ alkynyl c ~ 1-6 ~ alkyl, c ~ 3-8 ~ cycloalkyl, c ~ cycloalkyl 3-8 ~ C ~ 1-3 ~ alkyl, aryl C ~ 1-3 ~ alkyl or heteroaryl C ~ 1-3 ~ alkyl; r ^ 2 ^ represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring (a) attached to the rest of the molecule via one of the carbon atoms in the benzene ring and in which the fused ring ( a) it is a 5- or 6-membered ring that can be saturated or partially or completely unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulfur and nitrogen; r ^ 3 ^ represents hydrogen or c ~ 1 ~ - c ~ 3 ~ alkyl, or r ^ 1 ^ and r ^ 3 ^ together represent a 3 or 4 membered alkenyl or alkyl chain. a compound of the formula (i) is a potent and selective inhibitor of specific 3 ', 5' cyclic guanosine monophosphate (cgmp specific powder) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including treatment cardiovascular disorders.

BRPI9506559A 1994-01-21 1995-01-19 compounds of tetracyclic derivatives, cis isomer of tetracyclic derivatives, and pharmaceutical composition BR9506559C8 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9401090A GB9401090D0 (en) 1994-01-21 1994-01-21 Chemical compounds
PCT/EP1995/000183 WO1995019978A1 (en) 1994-01-21 1995-01-19 Tetracyclic derivatives, process of preparation and use

Publications (2)

Publication Number Publication Date
BR9506559A BR9506559A (en) 1997-10-28
BR9506559C8 true BR9506559C8 (en) 2020-07-07

Family

ID=10749089

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI9506559A BR9506559C8 (en) 1994-01-21 1995-01-19 compounds of tetracyclic derivatives, cis isomer of tetracyclic derivatives, and pharmaceutical composition

Country Status (49)

Country Link
US (5) US5859006A (en)
EP (1) EP0740668B1 (en)
JP (3) JP3808095B2 (en)
KR (1) KR100357411B1 (en)
CN (2) CN1045777C (en)
AP (1) AP556A (en)
AT (1) ATE169018T1 (en)
AU (2) AU689205B2 (en)
BG (1) BG62733B1 (en)
BR (1) BR9506559C8 (en)
CA (1) CA2181377C (en)
CO (1) CO4340684A1 (en)
CZ (1) CZ286566B6 (en)
DE (2) DE69503753T2 (en)
DK (1) DK0740668T3 (en)
EE (1) EE03231B1 (en)
EG (1) EG25852A (en)
ES (1) ES2122543T3 (en)
FI (1) FI113176B (en)
GB (1) GB9401090D0 (en)
HK (1) HK1013286A1 (en)
HR (1) HRP950023B1 (en)
HU (1) HU222494B1 (en)
IL (1) IL112384A (en)
IN (1) IN183942B (en)
IS (1) IS1888B (en)
LU (1) LU91017I2 (en)
LV (1) LV11690B (en)
MA (1) MA23433A1 (en)
MX (1) MX9602904A (en)
MY (1) MY114663A (en)
NL (1) NL300124I2 (en)
NO (2) NO306465B1 (en)
NZ (1) NZ279199A (en)
OA (1) OA10584A (en)
PE (1) PE49495A1 (en)
PL (1) PL179744B1 (en)
RO (1) RO117794B1 (en)
RU (1) RU2142463C1 (en)
SA (1) SA95150475B1 (en)
SG (1) SG49184A1 (en)
SI (1) SI0740668T1 (en)
SK (1) SK280879B6 (en)
SV (1) SV1995000002A (en)
TN (1) TNSN95004A1 (en)
TW (1) TW378210B (en)
UY (1) UY23893A1 (en)
WO (1) WO1995019978A1 (en)
ZA (1) ZA95424B (en)

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CN1070492C (en) 2001-09-05
CZ286566B6 (en) 2000-05-17
DE69503753T2 (en) 1999-01-21
HRP950023A2 (en) 1998-04-30
CA2181377C (en) 2002-05-28
IL112384A (en) 1998-08-16
HUT74943A (en) 1997-03-28
BR9506559A (en) 1997-10-28
SV1995000002A (en) 1995-10-04
AU689205B2 (en) 1998-03-26
JPH09508113A (en) 1997-08-19
NL300124I1 (en) 2003-07-01
CA2181377A1 (en) 1995-07-27
US6369059B1 (en) 2002-04-09
NZ279199A (en) 1998-01-26
SG49184A1 (en) 1998-05-18
SK280879B6 (en) 2000-08-14
IS1888B (en) 2003-09-01
AU707055B2 (en) 1999-07-01
PE49495A1 (en) 1996-01-10
AU7391298A (en) 1998-08-20
ES2122543T3 (en) 1998-12-16
KR100357411B1 (en) 2003-02-05

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